Taprostene (free acid)
(Synonyms: 他前列烯,CG-4203) 目录号 : GC44991Stable prostacyclin analog
Cas No.:108945-35-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >95.00%
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Taprostene is a stable prostacyclin (PGI2) analog and agonist of the prostacyclin receptor, IP. It does not activate the PGE2 receptor EP4, which, like IP, promotes vascular smooth muscle relaxation when stimulated. Taprostene has been used extensively to study the role of the IP receptor in tissue preparations and in vivo. It has also been used in the screening and evaluation of potential IP antagonists.
Cas No. | 108945-35-3 | SDF | |
别名 | 他前列烯,CG-4203 | ||
Canonical SMILES | O[C@@H]([C@@H]1/C=C/[C@H](O)C2CCCCC2)C[C@]([C@]1([H])C/3)([H])OC3=C/C4=CC=CC(C(O)=O)=C4 | ||
分子式 | C24H30O5 | 分子量 | 398.5 |
溶解度 | Water: 25 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.5094 mL | 12.5471 mL | 25.0941 mL |
5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL |
10 mM | 0.2509 mL | 1.2547 mL | 2.5094 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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The scavenging of hydroxyl radical(.OH) by a prostacyclin analogue, Taprostene
Chem Biol Interact 1994 Apr;91(1):29-38.PMID:8194123DOI:10.1016/0009-2797(94)90004-3.
A possible mechanism by which prostacyclin (PGI2) analogues provide beneficial effects including improved survival in shock experimentally induced by endotoxin, polytrauma or hypovolemia was studied. Since several studies have implicated oxygen free radical-mediated tissue damage, we investigated whether PGI2-analogues exert their 'cytoprotective' effects by inhibiting overproduction of oxygen free radicals. For this reason, the efficiency of Taprostene to scavenge hydroxyl radicals (.OH) and to possibly prevent the subsequent formation of reactive oxygen species was studied. Competition experiments were performed in which the .OH generated by H2O2/Fe2+ abstracted a hydrogen from Taprostene (CG-4203) [5Z,13E, 9,11,15S)-2,3,4-trinor-1,5-inter-m-phenylene-6,9-epoxy-11,15-di hyd roxy-15-cyclohexyl-16,17,18,19,20-pentanor-prosta-5,13-dieno ic acid sodium salt], and the resulting carbon-centered radical was trapped with the spin trap 3,3,5,5-tetramethyl-1-pyrroline-N-oxide (M4PO). This spin trap reacted with .OH to yield an M4PO-OH spin adduct observable by Electron Paramagnetic Resonance (EPR) spectroscopy and resulted in the rate constant, k2 = 1.5 x 10(10) M-1s-1, for the reaction between .OH and Taprostene. The results show that Taprostene is an efficient .OH scavenger. In addition, reactions of hypochlorous ion (-OCL) with hydrogen peroxide (H2O2) in the presence of Taprostene were monitored using the spin trap 5,5-dimethyl-1-pyrroline-N-oxide (DMPO) and M4PO dissolved in deuterium oxide.
Effects of Taprostene, a chemically stable prostacyclin analogue, in patients with ischaemic peripheral vascular disease: a placebo controlled double-blind trial
Prostaglandins Leukot Essent Fatty Acids 1989 Oct;38(1):31-5.PMID:2514430DOI:10.1016/0952-3278(89)90144-0.
Thirty patients with ischaemic peripheral vascular disease and intermittent claudication were randomly allocated to receive either placebo or Taprostene, a chemically stable prostacyclin analogue, intravenously at a rate of 25 ng/kg/min for 6 hours daily on 5 consecutive days. Taprostene produced a significant (p less than 0.05) increase in absolute walking time compared to placebo on one day after infusion and at 1, 4 and 8 weeks (14% vs 2.8%) later. Taprostene also produced a significant (p less than 0.05) increase in the pain-free walking time compared to placebo in the follow-up period (8 weeks after infusion: 23% vs 3.8%). During the infusion period systolic and diastolic blood pressure decreased (p less than 0.05) and heart rate was accelerated (p less than 0.05) in the Taprostene treated group whereas no change was monitored in the placebo group. The ankle/brachial Doppler index was unaffected by Taprostene. The platelet half-life was significantly (p less than 0.05) prolonged following taprostene-infusion (72.6 +/- 9.35 vs 77.9 +/- 7.44 hours). However, no change on platelet half-life was found in the placebo group (p less than 0.05). Various measures of platelet function parameters followed in vitro (ADP-induced aggregation, platelet sensitivity to PGI2, PGE1, PGD1 and Taprostene, concentrations of platelet factor 4 and beta-thromboglobulin) showed no change with Taprostene. Measures of circulating platelet aggregates and endothelial cells count showed no changes during the 2 months follow-up period too. It is assumed that Taprostene may be of clinical benefit in patients with ischaemic peripheral vascular disease. However, future investigations have to be carried out to assess the optimal dose regime.